2. Academic Validation
  3. Mycobacterial tryptophan biosynthesis: A promising target for tuberculosis drug development?

Mycobacterial tryptophan biosynthesis: A promising target for tuberculosis drug development?

  • Bioorg Med Chem Lett. 2019 Dec 1;29(23):126731. doi: 10.1016/j.bmcl.2019.126731.
Sara Consalvi 1,  Cristina Scarpecci 1,  Mariangela Biava 1,  Giovanna Poce 2
Affiliations

Affiliations

  • 1 Department of Chemistry and Technologies of Drug, Sapienza University of Rome, piazzale A. Moro 5, 00185 Rome, Italy.
  • 2 Department of Chemistry and Technologies of Drug, Sapienza University of Rome, piazzale A. Moro 5, 00185 Rome, Italy. Electronic address: giovanna.poce@uniroma1.it.
PMID: 31627992 DOI: 10.1016/j.bmcl.2019.126731
Abstract

The biosynthetic pathways of Amino acids are attractive targets for drug development against pathogens with an intracellular behavior like M. tuberculosis (Mtb). Indeed, while in the macrophages Mtb has restricted access to Amino acids such as tryptophan (Trp). Auxotrophic Mtb strains, with mutations in the Trp biosynthetic pathway, showed reduced intracellular survival in cultured human and murine macrophages and failed to cause the disease in immunocompetent and immunocompromised mice. Herein we present recent efforts in the discovery of Trp biosynthesis inhibitors.

Keywords

Drug discovery; Inhibitors; M. tuberculosis; Tryptophan; Tuberculosis.

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